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Studies in rabbits have shown peak concentrations of 20 ng/g of the free acid in aqueous humour one to two hours after topical dosing of Travoprost

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Academic year: 2022

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Travoprost/ Pharmathen 40 micrograms/mL preservative free eye drops, solution in multi dose container

2.2 Introduction, p.1

2.2 Introduction

International Nonproprietary Name (rINN): Travoprost Structural formula:

Molecular formula:

Molecular weight:

Chemical names:

Travoprost decrease the elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Travoprost, a prostaglandin F analogue, is a highly selective full agonist which has a high affinity for the prostaglandin FP receptor, and reduces the intraocular pressure by increasing the outflow of aqueous humour via trabecular meshwork and uveoscleral pathways. Reduction of the intraocular pressure in man starts about 2 hours after administration and maximum effect is reached after 12 hours. Significant lowering of intraocular pressure can be maintained for periods exceeding 24 hours with a single dose.

Data on adjunctive administration of Travoprost with timolol % and limited data with brimonidine % were collected during clinical trials that showed an additive effect of Travoprost with these glaucoma medications. No clinical data are available on adjunctive use with other ocular hypotensive medications.

Travoprost significantly increased optic nerve head blood flow in rabbits following 7 days of topical ocular administration (1.4 micrograms, once-daily)

Travoprost is an ester prodrug. It is absorbed through the cornea where the isopropyl ester is hydrolysed to the active free acid. Studies in rabbits have shown peak concentrations of 20 ng/g of the free acid in aqueous humour one to two hours after topical dosing of Travoprost. Aqueous humour concentrations declined with a half- life of approximately 1.5 hours.

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Travoprost/ Pharmathen 40 micrograms/mL preservative free eye drops, solution in multi dose container

2.2 Introduction, p.2

Following topical ocular administration of Travoprost to healthy volunteers, low systemic exposure to active free acid was demonstrated. Peak active free acid plasma concentrations of 25 pg/ml or less were observed between 10 and 30 minutes post- dose. Thereafter, plasma levels declined rapidly to below the 10 pg/ml assay quantitation limit before 1 hour post-administration. Due to the low plasma concentrations and rapid elimination following topical dosing, the elimination half- life of active free acid in man could not be determined.

Metabolism is the major route of elimination of both travoprost and the active free acid. The systemic metabolic pathways parallel those of endogenous prostaglandin F which are characterised by reduction of the 13-14 double bond, oxidation of the 15- hydroxyl and β-oxidative cleavages of the upper side chain.

Travoprost free acid and its metabolites are mainly excreted by the kidneys.

Travoprost has been studied in patients with mild to severe hepatic impairment and in patients with mild to severe renal impairment (creatinine clearance as low as 14 ml/min). No dosage adjustment is necessary in these patients.

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